CN103054888A - Solid oral preparation containing acarbose and atorvastatin calcium and preparation method of solid oral preparation - Google Patents
Solid oral preparation containing acarbose and atorvastatin calcium and preparation method of solid oral preparation Download PDFInfo
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- CN103054888A CN103054888A CN201210586812XA CN201210586812A CN103054888A CN 103054888 A CN103054888 A CN 103054888A CN 201210586812X A CN201210586812X A CN 201210586812XA CN 201210586812 A CN201210586812 A CN 201210586812A CN 103054888 A CN103054888 A CN 103054888A
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- acarbose
- atorvastatin calcium
- orally ingestible
- adjuvant
- solid orally
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- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 title claims abstract description 61
- OJRHUICOVVSGSY-RXMQYKEDSA-N (2s)-2-chloro-3-methylbutan-1-ol Chemical compound CC(C)[C@H](Cl)CO OJRHUICOVVSGSY-RXMQYKEDSA-N 0.000 title claims abstract description 58
- 229960002632 acarbose Drugs 0.000 title claims abstract description 57
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 title claims abstract description 57
- 229960001770 atorvastatin calcium Drugs 0.000 title claims abstract description 55
- 239000007787 solid Substances 0.000 title claims abstract description 31
- 238000002360 preparation method Methods 0.000 title claims abstract description 16
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 20
- 239000002671 adjuvant Substances 0.000 claims description 19
- 239000000203 mixture Substances 0.000 claims description 14
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 10
- 235000019359 magnesium stearate Nutrition 0.000 claims description 10
- 239000000741 silica gel Substances 0.000 claims description 10
- 229910002027 silica gel Inorganic materials 0.000 claims description 10
- 238000005303 weighing Methods 0.000 claims description 10
- 239000002775 capsule Substances 0.000 claims description 7
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 5
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 5
- 239000008101 lactose Substances 0.000 claims description 5
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 5
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 5
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 4
- 239000011734 sodium Substances 0.000 claims description 4
- 229910052708 sodium Inorganic materials 0.000 claims description 4
- 229920001353 Dextrin Polymers 0.000 claims description 3
- 239000004375 Dextrin Substances 0.000 claims description 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 3
- 229920002472 Starch Polymers 0.000 claims description 3
- 239000011230 binding agent Substances 0.000 claims description 3
- 235000019425 dextrin Nutrition 0.000 claims description 3
- 239000008187 granular material Substances 0.000 claims description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 3
- 229950005770 hyprolose Drugs 0.000 claims description 3
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- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 229950008138 carmellose Drugs 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 abstract description 20
- 239000008280 blood Substances 0.000 abstract description 20
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract description 20
- 235000012000 cholesterol Nutrition 0.000 abstract description 9
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 abstract description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract description 5
- 239000008103 glucose Substances 0.000 abstract description 5
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- 230000002218 hypoglycaemic effect Effects 0.000 abstract description 3
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- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
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- HIMXGTXNXJYFGB-UHFFFAOYSA-N alloxan Chemical compound O=C1NC(=O)C(=O)C(=O)N1 HIMXGTXNXJYFGB-UHFFFAOYSA-N 0.000 description 6
- 230000037396 body weight Effects 0.000 description 6
- 235000013361 beverage Nutrition 0.000 description 5
- 235000013305 food Nutrition 0.000 description 5
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 description 4
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 description 4
- 229960005370 atorvastatin Drugs 0.000 description 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 4
- 210000002966 serum Anatomy 0.000 description 4
- 230000000630 rising effect Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- CABVTRNMFUVUDM-VRHQGPGLSA-N (3S)-3-hydroxy-3-methylglutaryl-CoA Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCSC(=O)C[C@@](O)(CC(O)=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 CABVTRNMFUVUDM-VRHQGPGLSA-N 0.000 description 2
- 102000004877 Insulin Human genes 0.000 description 2
- 108090001061 Insulin Proteins 0.000 description 2
- 108090001030 Lipoproteins Proteins 0.000 description 2
- 102000004895 Lipoproteins Human genes 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- FQCKMBLVYCEXJB-MNSAWQCASA-L atorvastatin calcium Chemical compound [Ca+2].C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1.C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 FQCKMBLVYCEXJB-MNSAWQCASA-L 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 229940125396 insulin Drugs 0.000 description 2
- 229940002661 lipitor Drugs 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 235000021590 normal diet Nutrition 0.000 description 2
- 210000003462 vein Anatomy 0.000 description 2
- SRNWOUGRCWSEMX-UHFFFAOYSA-N Adenosine diphosphate ribose Natural products C1=NC=2C(N)=NC=NC=2N1C(C(C1O)O)OC1COP(O)(=O)OP(O)(=O)OCC1OC(O)C(O)C1O SRNWOUGRCWSEMX-UHFFFAOYSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 208000002249 Diabetes Complications Diseases 0.000 description 1
- 206010012655 Diabetic complications Diseases 0.000 description 1
- 108010001394 Disaccharidases Proteins 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 1
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 1
- 108010028554 LDL Cholesterol Proteins 0.000 description 1
- 102000000853 LDL receptors Human genes 0.000 description 1
- 108010001831 LDL receptors Proteins 0.000 description 1
- 102100024295 Maltase-glucoamylase Human genes 0.000 description 1
- BAWFJGJZGIEFAR-NNYOXOHSSA-N NAD zwitterion Chemical compound NC(=O)C1=CC=C[N+]([C@H]2[C@@H]([C@H](O)[C@@H](COP([O-])(=O)OP(O)(=O)OC[C@@H]3[C@H]([C@@H](O)[C@@H](O3)N3C4=NC=NC(N)=C4N=C3)O)O2)O)=C1 BAWFJGJZGIEFAR-NNYOXOHSSA-N 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a solid oral preparation containing acarbose and atorvastatin calcium. The solid oral preparation comprises acarbose and atorvastatin calcium, wherein the weight ratio of the acarbose to the atorvastatin calcium is (5-80): (20-200); and the solid oral preparation further comprises pharmaceutically acceptable excipients, wherein the weight ratio of the atorvastatin calcium to the excipients is 1: (2.3-30). The invention further discloses a preparation method of the solid oral preparation. The invention has the beneficial effects that the blood glucose and the blood lipids can be reduced synergistically, the cholesterol and triglyceride can be lowered while the blood glucose is reduced, the high-density lipoprotein (HDL) level in the blood can be increased, and the hypoglycemic and hypolipidemic effects can be improved, thereby correcting the metabolic syndrome of diabetics and reducing the long-term risk of cardiovascular and cerebrovascular diseases of the diabetics.
Description
Technical field
The present invention relates to the pharmaceutical preparations technology field, particularly contain solid orally ingestible of acarbose and Atorvastatin calcium and preparation method thereof.
Background technology
Acarbose is a kind of biosynthetic false tetrose, animal test results shows, acarbose is active inhibited to the alpha-glucosidase of small bowel cell brush border, thereby suppressed the degraded of polysaccharide, oligosaccharide or disaccharidase in the intestinal, make degraded and the absorbed into serum speed of the glucose of self-carbon water compound to slow down, reduced the rising of post-prandial glycemia, the average blood sugar value is descended.
Atorvastatin calcium is the selectivity that synthesizes in recent years, competitive 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, and effect for reducing fat is higher than other HMG-CoA reductase inhibitors.The non-activity of Atorvastatin calcium own, hydrolyzate after the oral absorption suppresses the rate-limiting enzyme HMG-CoA reductase in the cholesterol biosynthesis process in vivo competitively, make the synthetic minimizing of cholesterol, also make the synthetic increase of low density lipoprotein receptor, the Main Function position is at liver, the result reduces cholesterolemia and low-density lipoprotein cholesterol level, and moderate reduces serum triglyceride level and increases the blood hdl level.Thus to the control generation effect of atherosclerosis and coronary heart disease.
Summary of the invention
The object of the present invention is to provide a kind ofly has synergism to blood sugar lowering and blood fat reducing, can be at hypoglycemic while cholesterol reducing and triglyceride, and the solid orally ingestible that contains acarbose and Atorvastatin calcium and preparation method thereof of the effect of rising blood middle-high density lipoprotein levels is arranged.
Purpose of the present invention is achieved through the following technical solutions: contain the solid orally ingestible of acarbose and Atorvastatin calcium, it comprises Atorvastatin calcium and acarbose, and the weight ratio of Atorvastatin calcium and acarbose is:
Atorvastatin calcium 5～80,
Acarbose 20～200.
It also comprises pharmaceutically acceptable pharmaceutic adjuvant, the weight ratio of Atorvastatin calcium and adjuvant is 1:2.3～30, and described adjuvant comprises one or more in starch, lactose, PVP, dextrin, microcrystalline Cellulose, carmellose, carboxymethylstach sodium, hyprolose, micropowder silica gel, the magnesium stearate.
Described solid orally ingestible is capsule or tablet.
Each capsule or tablet contain Atorvastatin calcium 5mg～80mg, acarbose 20mg ~ 0.2g.
The described preparation method that contains the solid orally ingestible of acarbose and Atorvastatin calcium, it may further comprise the steps:
S1, take by weighing acarbose, Atorvastatin calcium and adjuvant by above-mentioned weight ratio, acarbose, Atorvastatin calcium are crossed 100 mesh sieves, and adjuvant is crossed 80 mesh sieves;
S2, with the component mix homogeneously of removing in acarbose, Atorvastatin calcium and the adjuvant outside PVP, micropowder silica gel and the magnesium stearate; The PVP that takes by weighing is mixed with 5% solution with pure water, and it is sprayed into the said mixture material as binding agent, be mixed to do and wet evenly, granulate with 16 ~ 24 mesh sieves;
S3, be dried to moisture below 5%, add the micropowder silica gel and the magnesium stearate that take by weighing, and mix homogeneously, be pressed into sheet or the encapsulated solid orally ingestible that contains acarbose and Atorvastatin calcium that namely gets
The present invention has the following advantages: the present invention has synergism to blood sugar lowering and blood fat reducing, can be at hypoglycemic while cholesterol reducing and triglyceride, and the effect of rising blood middle-high density lipoprotein levels is arranged; Improve blood sugar lowering, effect for reducing blood fat, be used for correcting the metabolism syndrome of diabetics, be conducive to reduce the cardiovascular and cerebrovascular disease danger at a specified future date of diabetics.
The specific embodiment
The present invention will be further described below in conjunction with embodiment, and protection scope of the present invention is not limited to the following stated:
Embodiment 1:
The solid orally ingestible that contains acarbose and Atorvastatin calcium can be tablet or capsule, and it comprises that following component and per 1000 (grain) consumptions of each component are:
Acarbose 20g,
Atorvastatin calcium 5g,
Adjuvant 150g,
Described adjuvant comprises following component, and the consumption of each component is:
Starch 20g,
Lactose 70g,
Microcrystalline Cellulose 40g,
Hyprolose 13g,
PVPK series 5g,
Magnesium stearate 2g.
Above-mentioned acarbose quality meets WS-(X-3157)-2004Z, and Atorvastatin calcium meets WS-(X-127)-2003Z.
Contain the preparation method of the solid orally ingestible of acarbose and Atorvastatin calcium, it may further comprise the steps:
S1, take by weighing acarbose, Atorvastatin calcium and adjuvant by above-mentioned prescription, acarbose, Atorvastatin calcium are crossed 100 mesh sieves, and adjuvant is crossed 80 mesh sieves;
S2, with the component mix homogeneously of removing in acarbose, Atorvastatin calcium and the adjuvant outside PVP, micropowder silica gel and the magnesium stearate; The PVP that takes by weighing is mixed with 5% solution with pure water, and it is sprayed into the said mixture material as binding agent, be mixed to do and wet evenly, granulate with 16 ~ 24 mesh sieves;
S3, be dried to moisture below 5%, add the micropowder silica gel and the magnesium stearate that take by weighing, and mix homogeneously, be pressed into sheet or the encapsulated solid orally ingestible that contains acarbose and Atorvastatin calcium that namely gets.
Embodiment 2:
The solid orally ingestible that contains acarbose and Atorvastatin calcium can be tablet or capsule, and it comprises that following component and per 1000 (grain) consumptions of each component are:
Acarbose 100g,
Atorvastatin calcium 23g,
Adjuvant 184g,
Described adjuvant comprises following component, and the consumption of each component is:
Dextrin 30g,
Lactose 70g,
Microcrystalline Cellulose 50g,
Carboxymethylstach sodium 20g,
PVPK series 10g,
Micropowder silica gel 4g.
Above-mentioned acarbose quality meets WS-(X-3157)-2004Z, and Atorvastatin calcium meets WS-(X-127)-2003Z.
Contain the preparation method of solid orally ingestible of acarbose and Atorvastatin calcium with embodiment 1.
Embodiment 3:
The solid orally ingestible that contains acarbose and Atorvastatin calcium can be tablet or capsule, and it comprises that following component and per 1000 (grain) consumptions of each component are:
Acarbose 200g,
Atorvastatin calcium 80g,
Adjuvant 184g,
Described adjuvant comprises following component, and the consumption of each component is:
Lactose 70g,
Microcrystalline Cellulose 60g,
Carboxymethylstach sodium 20g,
Hydroxyl methylcellulose 20g,
PVPK series 5g,
Micropowder silica gel (adding) 5g,
Magnesium stearate (adding) 4g.
Above-mentioned acarbose quality meets WS-(X-3157)-2004Z, and Atorvastatin calcium meets WS-(X-127)-2003Z.
Contain the preparation method of solid orally ingestible of acarbose and Atorvastatin calcium with embodiment 1.The present invention will be further described below in conjunction with test:
Animal: 90 of healthy SD male rats, body weight 200g ± 20g.
Experimental animal feedstuff: 1, normal feedstuff; 2, high lipid food: self-control forms: Adeps Sus domestica 30%+ cholesterol 1%+ normal feedstuff 69%, and the cholesterol addition is 149.5mg/kg; 3, alloxan aqueous solution 10mg/ml (PH3) faces and uses new system.
Medicine: 1, the solid orally ingestible that contains acarbose and Atorvastatin calcium of the present invention.
2, commercially available acarbose tablet (acarbose, specification 50mg, every heavy 0.14g, lot number: BJ06514, Bayer HealthCare Co) and commercially available atorvastatin (lipitor, specification 20mg, every heavy 0.16g, lot number: 038711K, lot number of the repackaged products: 1137057, pfizer inc).
Instrument and reagent: 1, triglyceride determination test kit, No. the 2400362nd, Beijing Kinghawk Pharmaceutical Co., Ltd.'s capital medicine prison tool (standard) word 2006.
2, No. the 2400356th, cholesterol determination test kit Beijing Kinghawk Pharmaceutical Co., Ltd. capital medicine prison tool (standard) word 2006.
3, stable blood glucose meter (No. the 2400069th, Hunan food medicine prison tool (standard) word 2008, unit special use BIDI28F0068) with test strip for blood-sugar (No. the 2400070th, Hunan food medicine prison tool (standard) word 2008, lot number: 2226NC), Changsha Sinocare Inc..
Experimental technique:
1, modeling
Rat is divided into the high sugared model group (n=80) of high fat, blank group (n=10) at random, the high sugared model group of high fat is pressed 100mg/kg lumbar injection alloxan every day, and (alloxan is by destroying insulin β cell, make cell DNA impaired, and the activity of activation adenosine diphosphate ribose body synzyme, make the cozymase content decrease, finally cause insulin deficit, make metabolism disorder, blood sugar increasing.), raise simultaneously with high lipid food; The blank group is raised with normal diet.Raised for 13 weeks continuously.
After continuously raising for 4 weeks, by U.S. diabetic complication model association (AMDCC) proposed standard, fasting 6 hours: 7 of mornings are got the blood point: get the about 0.4ml mensuration of ophthalmic corner of the eyes vein peripheral blood after the anesthesia to point at noons 13.Require: blood glucose (Glu) 11.1mmol/l is considered as the modeling success, has 71 modelings successes.
This patent effect: the present composition is on the impact of rat fat and cholesterol
2, test
The rat of modeling success is divided into embodiment of the invention group, acarbose group, Atorvastatin calcium group at random, the above-mentioned still conduct blank of blank group of modeling of not implementing is to group, raise with normal diet, embodiment of the invention group, acarbose group, Atorvastatin calcium group, when continuing to raise with high lipid food, give respectively embodiment of the invention compositions, acarbose tablet, atorvastatin, fed for 3 weeks continuously, each group is freely drunk water, itemized record are respectively organized daily ingestion amount, routine weighing in the process of the test.12h freely drinks water on an empty stomach before putting to death, and weighs, and the eye socket posterior vein is got hematometry.
Medication:
1 group of the embodiment of the invention: give simultaneously the solid orally ingestible that contains acarbose and Atorvastatin calcium that embodiment 1 makes raising with high fat beverage, press the 40mg/kg rat body weight.
2 groups of the embodiment of the invention: give simultaneously the solid orally ingestible that contains acarbose and Atorvastatin calcium that embodiment 2 makes raising with high fat beverage, press the 30mg/kg rat body weight.
3 groups of the embodiment of the invention: give simultaneously the solid orally ingestible that contains acarbose and Atorvastatin calcium that embodiment 3 makes raising with high fat beverage, press the 20mg/kg rat body weight.
Acarbose group: give simultaneously acarbose tablet raising with high fat beverage, press the 28mg/kg(acarbose) rat body weight.
Atorvastatin group: give simultaneously atorvastatin (lipitor) raising with high fat beverage, press the 8mg/kg rat body weight.
Results and analysis:
The invention compositions is on the impact of triglyceride in the rat blood serum (TG) and serum total cholesterol (TC), and result and analysis see the following form.
Annotate: refer to the index that records after the modeling in the table before the test, refer to medicine feed data measureds after 3 weeks after the test.
Above experimental data shows: the present composition (experimental example 1 ~ 3) test group and acarbose group and Atorvastatin calcium group more all there are differences, and there is significant difference P＜0.01, illustrate that subject composition has synergism to blood sugar lowering, blood fat reducing.
Claims (5)
1. contain the solid orally ingestible of acarbose and Atorvastatin calcium, it is characterized in that: it comprises Atorvastatin calcium and acarbose, and the weight ratio of Atorvastatin calcium and acarbose is:
Atorvastatin calcium 5～80,
Acarbose 20～200.
2. the solid orally ingestible that contains acarbose and Atorvastatin calcium according to claim 1, it is characterized in that: it also comprises pharmaceutically acceptable pharmaceutic adjuvant, the weight ratio of Atorvastatin calcium and adjuvant is 1:2.3～30, and described adjuvant comprises one or more in starch, lactose, PVP, dextrin, microcrystalline Cellulose, carmellose, carboxymethylstach sodium, hyprolose, micropowder silica gel, the magnesium stearate.
3. the solid orally ingestible that contains acarbose and Atorvastatin calcium according to claim 1, it is characterized in that: described solid orally ingestible is capsule or tablet.
4. the solid orally ingestible that contains acarbose and Atorvastatin calcium according to claim 3, it is characterized in that: each capsule or tablet contain Atorvastatin calcium 5mg～80mg, acarbose 20mg～0.2g.
5. the preparation method that contains the solid orally ingestible of acarbose and Atorvastatin calcium as claimed in claim 2, it is characterized in that: it may further comprise the steps:
S1, take by weighing acarbose, Atorvastatin calcium and adjuvant by above-mentioned weight ratio, acarbose, Atorvastatin calcium are crossed 100 mesh sieves, and adjuvant is crossed 80 mesh sieves;
S2, with the component mix homogeneously of removing in acarbose, Atorvastatin calcium and the adjuvant outside PVP, micropowder silica gel and the magnesium stearate; The PVP that takes by weighing is mixed with 5% solution with pure water, and it is sprayed into the said mixture material as binding agent, be mixed to do and wet evenly, granulate with 16 ~ 24 mesh sieves;
S3, be dried to moisture below 5%, add the micropowder silica gel and the magnesium stearate that take by weighing, and mix homogeneously, be pressed into sheet or the encapsulated solid orally ingestible that contains acarbose and Atorvastatin calcium that namely gets.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103127513A (en) * | 2013-03-11 | 2013-06-05 | 乔文龙 | Alpha-glycosidase inhibitor and hydroxymethyl glutaryl coenzyme A reductase inhibitor composition for treating diabetes and complications |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101590051A (en) * | 2008-05-29 | 2009-12-02 | 北京奥萨医药研究中心有限公司 | The pharmaceutical composition that contains nicotinic acid, HMG-CoA reductase inhibitor and alpha-glucosidase inhibitor |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101590051A (en) * | 2008-05-29 | 2009-12-02 | 北京奥萨医药研究中心有限公司 | The pharmaceutical composition that contains nicotinic acid, HMG-CoA reductase inhibitor and alpha-glucosidase inhibitor |
Non-Patent Citations (1)
| Title |
|---|
| ALAWI A,ET AL: "Risk of Adverse Events With Concomitant Use of Atorvastatin or Simvastatin and Glucose-Lowering Drugs (Thiazolidinediones, Metformin, Sulfonylurea,Insulin, and Acarbose)", 《THE AMERICAN JOURNAL OF CARDIOLOGY》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103127513A (en) * | 2013-03-11 | 2013-06-05 | 乔文龙 | Alpha-glycosidase inhibitor and hydroxymethyl glutaryl coenzyme A reductase inhibitor composition for treating diabetes and complications |
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